Publikationen

2025
Highly potent quinoxalinediones inhibit alpha-hemolysin and ameliorate Staphylococcus aureus lung infections

Shekhar A, Di Lucrezia R, Jerye K, Korotkov V S, Harmrolfs K, Rox K, Weich H A, Ghai I, Delhommel F, Becher I, Degenhart C, Fansa E, Unger A, Habenberger P, Klebl B, Lukat P, Schmelz S, Henke S, Borgert S, Lang J C, Sasse F, Diestel R, Richter C, Schneider-Daum N, Hinkelmann B, Niemz J, Lehr C M, Jansch L, Huehn J, Alm R, Savitski M, Welte T, Hesterkamp T, Sattler M, Winterhalter M, Blankenfeldt W, Medina E, Bilitewski U, Dinkel K and Bronstrup M. Cell Host Microbe. 2025; 33 (4): 560-572 e521. doi: 10.1016/j.chom.2025.03.006

The P2X7R-antagonist AFC-5128 ameliorates chronic experimental autoimmune encephalomyelitis in a preventive and therapeutic paradigm

Hoffrogge R, Karachunskaya A, Heitmann N, Pedreiturria X, Kloster K, Bader V, Winklhofer K F, Hamacher M, Klebl B, Gold R, Dinkel K, Kleiter I and Faissner S. Front Immunol. 2025; 16 1554999. doi: 10.3389/fimmu.2025.1554999

Design and Synthesis of Pyridine-Based Pyrrolo[2,3-d]pyrimidine Analogs as CSF1R Inhibitors: Molecular Hybridization and Scaffold Hopping Approach

Cherukupalli S, Degenhart C, Habenberger P, Unger A, Eickhoff J, Hoff B H and Sundby E. Pharmaceuticals. 2025; 18 (6): doi: 10.3390/ph18060814

P2X7R antagonism suppresses long-lasting hyperexcitability following traumatic brain injury in mice

Alves M, de Diego-Garcia L, Vegliante G, Moreno O, Gil B, Ramos-Cabrer P, Mitra M, Fernandez Martin A, Menendez Mendez A, Wang Y, Ryzwesky Strogulsky N, Sun M, Melia C, Conte G, Plaza-Garcia S, Khalin I, Teng X, Plesnila N, Klebl B, Dinkel K, Hamacher M, Bhattarcharya A, Ceusters M, Palmer J, Loane D, Llop J, Henshall D and Engel T. Theranostics. 2025; 15 (4): 1399-1419. doi: 10.7150/thno.97254

2024
Development of a live cell assay for real-time monitoring the interactions between the Hippo pathway components 14-3-3 and TAZ

Andlovic B, Wolf A, Hiltmann M, Klebl B M, Eickhoff J and Ottmann C. SLAS Discov. 2024; 29 (8): 100191. doi: 10.1016/j.slasd.2024.100191

TRPC5 controls the adrenaline-mediated counter regulation of hypoglycemia

Broker-Lai J, Rego Terol J, Richter C, Mathar I, Wirth A, Kopf S, Moreno-Perez A, Buttner M, Tan L L, Makke M, Poschet G, Hermann J, Tsvilovskyy V, Haberkorn U, Wartenberg P, Susperreguy S, Berlin M, Ottenheijm R, Philippaert K, Wu M, Wiedemann T, Herzig S, Belkacemi A, Levinson R T, Agarwal N, Camacho Londono J E, Klebl B, Dinkel K, Zufall F, Nussbaumer P, Boehm U, Hell R, Nawroth P, Birnbaumer L, Leinders-Zufall T, Kuner R, Zorn M, Bruns D, Schwarz Y and Freichel M. EMBO J. 2024; doi: 10.1038/s44318-024-00231-0

Understanding the Cytomegalovirus Cyclin-Dependent Kinase Ortholog pUL97 as a Multifaceted Regulator and an Antiviral Drug Target

Marschall M, Schutz M, Wild M, Socher E, Wangen C, Dhotre K, Rawlinson W D and Sticht H. Cells. 2024; 13 (16): doi: 10.3390/cells13161338

Inhibition of mammalian mtDNA transcription acts paradoxically to reverse diet-induced hepatosteatosis and obesity

Jiang S, Yuan T, Rosenberger F A, Mourier A, Dragano N R V, Kremer L S, Rubalcava-Gracia D, Hansen F M, Borg M, Mennuni M, Filograna R, Alsina D, Misic J, Koolmeister C, Papadea P, de Angelis M H, Ren L, Andersson O, Unger A, Bergbrede T, Di Lucrezia R, Wibom R, Zierath J R, Krook A, Giavalisco P, Mann M and Larsson N G. Nat Metab. 2024; 6 (6): 1024-1035. doi: 10.1038/s42255-024-01038-3

Fragment-Based Interrogation of the 14-3-3/TAZ Protein-Protein Interaction

Andlovic B, Valenti D, Centorrino F, Picarazzi F, Hristeva S, Hiltmann M, Wolf A, Cantrelle F X, Mori M, Landrieu I, Levy L M, Klebl B, Tzalis D, Genski T, Eickhoff J and Ottmann C. Biochemistry. 2024; 63 (17): 2196-2206. doi: 10.1021/acs.biochem.4c00248

An Antiherpesviral Host-Directed Strategy Based on CDK7 Covalently Binding Drugs: Target-Selective, Picomolar-Dose, Cross-Virus Reactivity

Yu D, Wagner S, Schutz M, Jeon Y, Seo M, Kim J, Bruckner N, Kicuntod J, Tillmanns J, Wangen C, Hahn F, Kaufer B B, Neipel F, Eickhoff J, Klebl B, Nam K and Marschall M. Pharmaceutics. 2024; 16 (2): doi: 10.3390/pharmaceutics16020158

Profiling of ERBB receptors and downstream pathways reveals selectivity and hidden properties of ERBB4 antagonists

Popović L, Wintgens J P, Wu Y, Brankatschk B, Menninger S, Degenhart C, Jensen N, Wichert S P, Klebl B, Rossner M J and Wehr M C. iScience. 2024; doi: 10.1016/j.isci.2024.108839

Pyrrolopyrimidine based CSF1R inhibitors: Attempted departure from Flatland

Bjornstad F, Havik S, Aarhus T I, Mahdi I, Unger A, Habenberger P, Degenhart C, Eickhoff J, Klebl B M, Sundby E and Hoff B H. Eur J Med Chem. 2024; 265 116053. doi: 10.1016/j.ejmech.2023.116053

Avapritinib-based SAR studies unveil a binding pocket in KIT and PDGFRA

Teuber A, Schulz T, Fletcher B S, Gontla R, Muhlenberg T, Zischinsky M L, Niggenaber J, Weisner J, Kleinbolting S B, Lategahn J, Sievers S, Muller M P, Bauer S and Rauh D. Nat Commun. 2024; 15 (1): 63. doi: 10.1038/s41467-023-44376-8